Velpandian Thirumurthy, Narayanan Kanniapan, Nag Tapas Chandra, Ravi Alok Kumar, Gupta Suresh Kumar
Ocular Pharmacology Division, Dr. Rajendra Prasad Centre for Ophthalmic Sciences, All India Institute of Medical Sciences, New Delhi, India.
Indian J Ophthalmol. 2006 Dec;54(4):237-40. doi: 10.4103/0301-4738.27947.
Candidal endophthalmitis is a sight-threatening ocular infection that most frequently occurs as a complication of candidemia. Fluconazole has been effective against Candida albicans in various animal models. Our objective was to evaluate retinal toxicity of plain and liposome formulation of fluconazole at various dose levels after intravitreal injection.
Twelve New Zealand albino rabbits weighing 2-2.5 kg were used. Two rabbits were used for every dose level. Liposome formulation containing 100 and 200 microg of fluconazole in sterile phosphate buffer solution and plain fluconazole at concentrations of 100, 200, 400 and 800 microg in 0.1 ml of sterile normal saline were injected intravitreally into the right eyes. The left eyes received 0.1 ml normal saline or 0.1 ml of liposome formulation without fluconazole. One week later, the animals were sacrificed, their eyes enucleated and processed for light microscopy and scanning electron microscopy.
It showed that plain fluconazole at a concentration of 100 microg and above caused retinal changes, with disorganization of the photoreceptor outer segments. However, liposome formulation of fluconazole (200 microg/0.1 ml) did not show any significant microscopic changes of the retina.
The liposome formulation decreased the retinal toxicity of fluconazole up to the studied concentration of 200 microg/0.1 ml.
念珠菌性眼内炎是一种威胁视力的眼部感染，最常作为念珠菌血症的并发症出现。氟康唑在各种动物模型中对白色念珠菌有效。我们的目的是评估玻璃体内注射后不同剂量水平的普通氟康唑和脂质体制剂的视网膜毒性。
使用12只体重2 - 2.5千克的新西兰白化兔。每个剂量水平使用两只兔子。将含有100和200微克氟康唑的脂质体制剂溶解于无菌磷酸盐缓冲溶液中，以及将浓度为100、200、400和800微克的普通氟康唑溶解于0.1毫升无菌生理盐水中，分别玻璃体内注射到右眼。左眼注射0.1毫升生理盐水或不含氟康唑的0.1毫升脂质体制剂。一周后，处死动物，摘除眼球并进行光学显微镜和扫描电子显微镜检查。
结果显示，浓度为100微克及以上的普通氟康唑会引起视网膜变化，感光细胞外节结构紊乱。然而，氟康唑脂质体制剂（200微克/0.1毫升）未显示视网膜有任何明显的微观变化。
在所研究的浓度达200微克/0.1毫升时，脂质体制剂降低了氟康唑的视网膜毒性。
